2c6c

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:2c6c.gif|left|200px]]
[[Image:2c6c.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 2c6c |SIZE=350|CAPTION= <scene name='initialview01'>2c6c</scene>, resolution 2.00&Aring;
+
The line below this paragraph, containing "STRUCTURE_2c6c", creates the "Structure Box" on the page.
-
|SITE= <scene name='pdbsite=AC1:24i+Binding+Site+For+Chain+A'>AC1</scene>
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=24I:(2S)-2-{[HYDROXY(4-IODOBENZYL)PHOSPHORYL]METHYL}PENTANEDIOIC+ACID'>24I</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=MAN:ALPHA-D-MANNOSE'>MAN</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Glutamate_carboxypeptidase_II Glutamate carboxypeptidase II], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.17.21 3.4.17.21] </span>
+
or leave the SCENE parameter empty for the default display.
-
|GENE=
+
-->
-
|DOMAIN=
+
{{STRUCTURE_2c6c| PDB=2c6c | SCENE= }}
-
|RELATEDENTRY=
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2c6c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2c6c OCA], [http://www.ebi.ac.uk/pdbsum/2c6c PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2c6c RCSB]</span>
+
-
}}
+
'''MEMBRANE-BOUND GLUTAMATE CARBOXYPEPTIDASE II (GCPII) IN COMPLEX WITH GPI-18431 (S)-2-(4-IODOBENZYLPHOSPHONOMETHYL)-PENTANEDIOIC ACID'''
'''MEMBRANE-BOUND GLUTAMATE CARBOXYPEPTIDASE II (GCPII) IN COMPLEX WITH GPI-18431 (S)-2-(4-IODOBENZYLPHOSPHONOMETHYL)-PENTANEDIOIC ACID'''
Line 34: Line 31:
[[Category: Slusher, B S.]]
[[Category: Slusher, B S.]]
[[Category: Tsukamoto, T.]]
[[Category: Tsukamoto, T.]]
-
[[Category: alternative splicing]]
+
[[Category: Alternative splicing]]
-
[[Category: antigen]]
+
[[Category: Antigen]]
-
[[Category: carboxypeptidase]]
+
[[Category: Carboxypeptidase]]
-
[[Category: dipeptidase]]
+
[[Category: Dipeptidase]]
-
[[Category: glycoprotein]]
+
[[Category: Glycoprotein]]
-
[[Category: hydrolase]]
+
[[Category: Hydrolase]]
-
[[Category: metal-binding]]
+
[[Category: Metal-binding]]
-
[[Category: metalloprotease]]
+
[[Category: Metalloprotease]]
-
[[Category: multifunctional enzyme]]
+
[[Category: Multifunctional enzyme]]
-
[[Category: naaladase]]
+
[[Category: Naaladase]]
-
[[Category: neurodegenerative disease]]
+
[[Category: Neurodegenerative disease]]
-
[[Category: peptidase]]
+
[[Category: Peptidase]]
-
[[Category: polymorphism]]
+
[[Category: Polymorphism]]
-
[[Category: prostate cancer]]
+
[[Category: Prostate cancer]]
-
[[Category: psma]]
+
[[Category: Psma]]
-
[[Category: signal-anchor]]
+
[[Category: Signal-anchor]]
-
[[Category: transmembrane]]
+
[[Category: Transmembrane]]
-
[[Category: zinc]]
+
[[Category: Zinc]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 21:19:38 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:17:01 2008''
+

Revision as of 18:19, 3 May 2008

Image:2c6c.gif

Template:STRUCTURE 2c6c

MEMBRANE-BOUND GLUTAMATE CARBOXYPEPTIDASE II (GCPII) IN COMPLEX WITH GPI-18431 (S)-2-(4-IODOBENZYLPHOSPHONOMETHYL)-PENTANEDIOIC ACID


Overview

Membrane-bound glutamate carboxypeptidase II (GCPII) is a zinc metalloenzyme that catalyzes the hydrolysis of the neurotransmitter N-acetyl-L-aspartyl-L-glutamate (NAAG) to N-acetyl-L-aspartate and L-glutamate (which is itself a neurotransmitter). Potent and selective GCPII inhibitors have been shown to decrease brain glutamate and provide neuroprotection in preclinical models of stroke, amyotrophic lateral sclerosis, and neuropathic pain. Here, we report crystal structures of the extracellular part of GCPII in complex with both potent and weak inhibitors and with glutamate, the product of the enzyme's hydrolysis reaction, at 2.0, 2.4, and 2.2 A resolution, respectively. GCPII folds into three domains: protease-like, apical, and C-terminal. All three participate in substrate binding, with two of them directly involved in C-terminal glutamate recognition. One of the carbohydrate moieties of the enzyme is essential for homodimer formation of GCPII. The three-dimensional structures presented here reveal an induced-fit substrate-binding mode of this key enzyme and provide essential information for the design of GCPII inhibitors useful in the treatment of neuronal diseases and prostate cancer.

About this Structure

2C6C is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure of glutamate carboxypeptidase II, a drug target in neuronal damage and prostate cancer., Mesters JR, Barinka C, Li W, Tsukamoto T, Majer P, Slusher BS, Konvalinka J, Hilgenfeld R, EMBO J. 2006 Mar 22;25(6):1375-84. Epub 2006 Feb 9. PMID:16467855 Page seeded by OCA on Sat May 3 21:19:38 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2c6c"
Personal tools